摘要
4-氟异喹啉-5-磺酰氯与(S)-2-氨基-N-(叔丁氧羰基)-N-(3-叔丁基二甲基硅烷氧基丙基)丙胺发生偶联反应,经TBAF脱去羟基保护后通过Mitsunobu反应自身环合,最后脱氨基保护得到青光眼治疗药物ripasudil,总收率31.3%。
Ripasudil was synthesized from 4-fluoroisoquinoline-5-sulfonyl chloride by coupling reaction with(S)-2-amino-N-(tert-butoxycarbonyl)-N-(3-tert-butyldimethylsilyloxypropyl)propylamine,then subjected to hydroxy deprotection with TBAF and then Mitsunobu reaction,followed by Boc deprotection with an overall yield of about 31.3%.
引文
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